Assay Detail

CHEMBL4616776

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Binding

Inhibition of BTK in human memory B cells assessed as reduction in CD86 surface expression

ChEMBL ↗

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Target

Tyrosine-protein kinase BTK (CHEMBL5251) ↗

Open DB target context

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Tyrosine-protein kinase BTK (CHEMBL5251) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Tyrosine-protein kinase BTK

CHEMBL5251

Anchored from Assay target.

Protein identity Tyrosine-protein kinase BTK

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Binding
Organism	Homo sapiens
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Tyrosine-protein kinase BTK (CHEMBL5251) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Discovery of Branebrutinib (BMS-986195): A Strategy for Identifying a Highly Potent and Selective Covalent Inhibitor Providing Rapid in Vivo Inactivation of Bruton's Tyrosine Kinase (BTK).

Watterson SH, Liu Q, Beaudoin Bertrand M, Batt DG, Li L, Pattoli MA, Skala S, Cheng L, Obermeier MT, Moore R, Yang Z, Vickery R, Elzinga PA, Discenza L, D'Arienzo C, Gillooly KM, Taylor TL, Pulicicchio C, Zhang Y, Heimrich E, McIntyre KW, Ruan Q, Westhouse RA, Catlett IM, Zheng N, Chaudhry C, Dai J, Galella MA, Tebben AJ, Pokross M, Li J, Zhao R, Smith D, Rampulla R, Allentoff A, Wallace MA, Mathur A, Salter-Cid L, Macor JE, Carter PH, Fura A, Burke JR, Tino JA.
J Med Chem (2019) 62 : 3228 -3250
PubMed 30893553 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	1	9.05	9.05

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL4297674	BRANEBRUTINIB	2.0	1	9.05

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL4297674	BRANEBRUTINIB	IC50	=	0.9	nM	9.05